Immediate release formulations of cinacalcet

Abstract

The invention relates to pharmaceutical compositions comprising: (a) from 15 to 50% by weight cinacalcet HCl; (b) from 30 to 80% by weight of one or more fillers; (c) from 5.1% to 7% by weight of one or more binders; and optionally one or more disintegrants, one or more glidants and/or one or more lubricants or one or more other acceptable pharmaceutical excipients and to a manufacturing process for the manufacture of such pharmaceutical compositions.

1 . A pharmaceutical composition, comprising:
 (a) from 15 to 50% by weight cinacalcet HCl;   (b) from 30 to 80% by weight of one or more fillers; and   (c) from 5.1% to 7% by weight of one or more binders;   and optionally one or more disintegrants, one or more glidants and/or one or more lubricants or one or more other acceptable pharmaceutical excipients,   wherein each percentage by weight is relative to the total weight of the composition.   
     
     
         2 . Pharmaceutical composition according to  claim 1 , comprising:
 (b) from 35% to 70% by weight of one or more fillers.   
     
     
         3 . Pharmaceutical composition according to  claim 1 , further comprising:
 (d) from 10.1% to 15% by weight of one or more disintegrants.   
     
     
         4 . Pharmaceutical composition according to  claim 1 , comprising:
 (a) from 18% to 45% by weight cinacalcet HCl;   (b) from 35% to 64% by weight of one or more fillers;   (c) from 5.1% to 7% by weight of one or more binders; and   (d) from 10.1% to 12% by weight of one or more disintegrants.   
     
     
         5 . Pharmaceutical composition according to  claim 1 , comprising:
 (a) from 18% to 20% by weight cinacalcet HCl;   (b) from 60% to 64% by weight of one or more fillers;   (c) from 5.1% to 7% by weight of one or more binders; and   (d) from 10.1% to 12% by weight of one or more disintegrants.   
     
     
         6 . Pharmaceutical composition according to  claim 1 , comprising:
 (a) from 41% to 44% by weight cinacalcet HCl;   (b) from 35% to 40% by weight of one or more fillers;   (c) from 5.1% to 7% by weight of one or more binders; and   (d) from 10.1% to 12% by weight of one or more disintegrants.   
     
     
         7 . Pharmaceutical composition according to  claim 4 , comprising:
 (d) from 10.5% to 11.5% by weight of one or more disintegrants.   
     
     
         8 . Pharmaceutical composition according to  claim 1 , comprising an intragranular phase, comprising:
 (a) from 18% to 20% by weight cinacalcet HCl;   (b′) from 30% to 40% by weight of one or more fillers;   (c) from 5.1% to 7% by weight of one or more binders; and   (d′) from 5% to 6% by weight of one or more disintegrants;   and an extragranular phase, comprising:   (b″) from 25% to 28% by weight of one or more fillers;   (d″) from 5% to 6% by weight of one or more disintegrants; and   (e) from 0.2% to 1% by weight of one or more glidants.   
     
     
         9 . Pharmaceutical composition according to  claim 1 , comprising an intragranular phase, comprising:
 (a) from 41% to 44% by weight cinacalcet HCl;   (b′) from 25% to 30% by weight of one or more fillers;   (c) from 5.1% to 7% by weight of one or more binders; and   (d′) from 5% to 6% by weight of one or more disintegrants;   
       and an extragranular phase, comprising:
 (b″) from 8% to 12% by weight of one or more fillers; 
 (d″) from 5% to 6% by weight of one or more disintegrants; and 
 (e) from 0.2% to 1% by weight of one or more glidants. 
 
     
     
         10 . Pharmaceutical composition according to  claim 1 , comprising:
 (c) from 5.5% to 6.5% by weight of one or more binders.   
     
     
         11 . Pharmaceutical composition according to  claim 1 , comprising:
 (f) from 0.2% to 1.5% by weight of one or more lubricants.   
     
     
         12 . Pharmaceutical composition according to  claim 1 , wherein the cinacalcet HCl particles exhibits a D 50  ranging from 5 μm to 95 μm. 
     
     
         13 . A process for the manufacture of a pharmaceutical composition comprising cinacalcet HCl according to  claim 1 , comprising the following steps:
 (a) mixing cinacalcet HCl, the binders, a portion of the fillers and a portion of the disintegrants to form an intragranular phase;   (b) wet granulating the intragranular phase to form wet granules;   (c) sieving the wet granules;   (d) drying the wet granules and calibrating the dried granules;   (e) mixing and sieving the remaining portions of fillers and disintegrants with the glidants to form an extragranular phase;   (f) blending the extragranular phase with the dried granules;   (g) sieving the lubricants and blend them with the mixture of dried granules and the extragranular phase to form the final blend which is used for production of the tablets.   
     
     
         14 . A method of treating secondary hyperparathyroidism resulting from chronical kidney insufficiency in a patient in need thereof, said method comprising administering said patient a pharmaceutical composition according to  claim 1 . 
     
     
         15 . A method of treating hypercalcaemia in patients with parathyroid carcinoma, said method comprising administering said patient a pharmaceutical composition according to  claim 1 .